Improving anti-tumor activity of sorafenib tosylate by lipid- and polymer-coated nanomatrix

• Main Authors: Yang Guo, Ting Zhong, Xiao-Chuan Duan, Shuang Zhang, Xin Yao, Yi-Fan Yin, Dan Huang, Wei Ren, Qiang Zhang, Xuan Zhang
• Format: Article
• Language: English
• Published: Taylor & Francis Group 2017-01-01
• Series: Drug Delivery
• Subjects: sorafenib tosylate; nanomatrix; poorly water-soluble drugs; bioavailability; anti-tumor activity
• Online Access: http://dx.doi.org/10.1080/10717544.2016.1245371
• ISSN: 1071-7544; 1521-0464

In the present study, we select the Sylysia 350 (Sylysia) as mesoporous material, distearoylphosphatidylethanolamine-poly(ethylene glycol)2000 (DSPE-PEG) as absorption enhancer and hydroxy propyl methyl cellulose (HPMC) as crystallization inhibitor to prepare sorafenib tosylate (SFN) nanomitrix (MSNM@SFN) for improving the anti-tumor activity of SFN. The MSNM@SFN was prepared by solvent evaporation method. The solubility, dissolution, and bioavailability of SFN in MSNM@SFN were also investigated. The anti-tumor activity of MSNM@SFN was evaluated in vitro and in vivo. Our results indicated that the solubility and dissolution of SFN in MSNM@SFN were significantly increased. The oral bioavailability of SFN in MSNM@SFN was greatly improved 7.7-fold compared with that in SFN suspension. The enhanced anti-tumor activity of MSNM@SFN was confirmed in vitro and in vivo experiments. This nanomatrix developed in this study could be a promising drug delivery platform for improving the therapeutic efficacy of poorly water-soluble drugs.